1. Field of the Invention
The present invention relates to sucralfate paste for use in treating mucosal lesions, and more particularly pertains to a sucralfate paste which is created through an incomplete reaction with acid prior to administration to a patient.
2. Description of Related Art
The use of sucralfate for the treatment of ulcers is known in the art. For example, in his letter to the editor in American Family Physician, January 1995, B. C. Demoss, M.D. contemplates the use of sucralfate tables (Carafate) in treating aphthous ulcers.
Sucralfate gel suspensions have also been employed as an antiulcerative drug. See S. Rossi et al., Rheological Study of Sucralfate Humid Gel: a Contribution to the Comprehension of its Stability Properties, Eur. J. Pharm. Biopharm. 1992:38:78-81.
The use of sucralfate gels as an ulcer healing drug has been detailed in other journals as well. See M. Guslandi et al., Effect of a Gel Formulation of Sucralfate on Gastric Microcirculation, J. Int""l Med. Res. 1993;21: 47-50; see also M. Miglioli, Prevention with Sucralfate Gel of NSAID-Induced Gastroduodenal Damage in Arthritic Patients, Am. J. Gastroenerology, Vol. 91, No. 11, 1996; D. Vaira, Gastric Retention of Sucralfate Gel and Suspension in Upper Gastrointestinal Diseases, Aliment Pharmacol Ther. 1993;7:531-535.
Lastly, U.S. Pat. No. 3,432,489 to Yoshihiro et al. discloses a disaccharide polysulfate-aluminum compound for use as a peptic ulcer inhibitor.
None of these disclosures, however, contemplates the advantageous effects of administration of sucralfate only after controlled incomplete reaction with acid. A result of this process is the production of a paste which is suitable for use without further pharmaceutical processing and which is fully biologically active at the time of application.
Consequently, it can be appreciated that there exists a continuing need for new and improved sucralfate compositions which can be used for the treatment of oral lesions. In this regard, the present invention substantially fulfills this need.
The general purpose of the present invention is to provide a compound which is especially effective in treating lesions.
To attain this, the present invention essentially comprises a compound consisting essentially of sucralfate incompletely dissolved within an acid.
It is therefore an object of the present invention to provide a novel sucralfate composition for the treatment of oral lesions.
It is another object of the present invention to provide a sucralfate paste which is created by the incomplete reaction of sucralfate with an acid.
It is a further object of the present invention to provide an acid activated product for greater efficiency in controlling lesions.
An even further object of the present invention is to provide efficient methods of producing the advantageous paste of the present invention.
Lastly, it is an object of the present invention to provide a method of treating open oral lesions comprising the following steps. First, providing approximately 5 grams of sucralfate and between 2 and 8 millimoles of HCl in a concentration greater than or equal to 0.1N. Thereafter, reacting the sucralfate within the HCl in a controlled manner whereby the sucralfate is polymerized but the complete dissolution of the sucralfate is prevented. Next, triturating the mixture into a smooth mass of paste and rinsing the resulting paste of excess acid. Finally, applying a portion of the paste to an open oral lesion.
It is therefore an object of the present invention to provide a sucralfate composition for the treatment of oral lesions.
The present invention relates to a sucralfate composition which is employed in the treatment of lesions. The composition is formed by the incomplete reaction between sucralfate and hydrochloric acid (HC1). The present invention contemplates various methods of achieving this incomplete reaction. In one example, a volume of sucralfate is mixed with hydrochloric acid of a select concentration. In additional examples, the sucralfate is first wetted in water before being mixed with the hydrochloric acid. Still yet another example involves mixing a volume of sucralfate powder with a powdered excipient before being mixed with the hydrochloric acid. The remaining detailed description provides more complete examples of sucralfate compositions, as well as their method of manufacture.
Sucralfate is an aluminum hydroxide salt of sucrose octasulfate. It is soluble in strong acid and strong alkali but is insoluble in most polar and non-polar solvents. Sucralfate is known to react with hydrochloric, sulfuric and other acids to form an amorphous paste. The present invention concerns the discovery that healing of oral mucosal lesions can be greatly accelerated if sucralfate is administered as a paste rather than a slurry. Although oral lesions are specified, the compound of the present invention can also be used for the treatment of lesions of the skin, esophagus, rectum, or any other like tissues.
The paste of the present invention is prepared by the incomplete reaction of sucralfate with acid, such a hydrochloric or sulfuric acid. By virtue of the incomplete reaction, no further pharmaceutical processing steps are needed. The incomplete reaction yields a fully biologically active compound.
The incomplete reaction is achieved through providing enough acid to produce significant sucralfate polymerization, while at the same time restricting the total acid availability so as to prevent complete dissolution of the drug. Experimentation has revealed that it is ideal to react approximately 5 grams of sucralfate with between 2 and 8 millimoles of HCl at a concentration of greater than or equal to 0.1N. Larger volumes of more concentrated acid, however, can also be used. Further, greater quantities of sucralfate and HCl can be employed to yield larger quantities of paste.
For example, 1.0 HCl can be employed in producing the desired compound. When 1.0N HCl is employed the surface area of contact between the sucralfate and acid must be increased to prevent an initial polymerization reaction at the surface of the powdered sucralfate from slowing the rate of polymerization deeper within the powdered sucralfate. This is achieved by first wetting the sucralfate within a volume of water to produce a slurry. Thereafter, the slurry is reacted with the 1.0N HCl.
In another example, the surface area of contact is increased by employing a powdered pharmaceutical excipient to include: povidone (PVP), talc, or others. Thereafter, the resulting powdered mixture is reacted with the 1.0N HCl. Other examples include an active agent composition with the excipient powder. Such active agents may include local anesthetics, antibiotics or compound stabilizers. Through the use of such active agents, beneficial results, beyond the specific activity of sucralfate can be achieved.
Whichever method of producing the paste compound of the present invention is utilized, subsequent transfer to an affected region can be achieved in any number of ways. Paste may be applied by direct transfer from finger to lesion, or via an applicator of plastic or other suitable material. Additionally, transfer may be facilitated by the transfer of a portion of paste first to the tip of the tongue, with subsequent transfer from the tongue to an oral lesion.
A kit designed to facilitate the preparation, dispensing and use of sucralfate paste may be created by incorporation of various applicators along with measured quantities of acid and with sucralfate powder premeasured into a vessel. The vessel could be used for both executing the acid reaction and the dispensing of the resulting medication.